IP Library Granted Patent US 11,485,753
Granted Patent B2
US 11,485,753 · App. 17/063,545 · Granted Nov 1, 2022

Substituted nucleosides, nucleotides and analogs thereof

Inventors: Leonid Beigelman (San Mateo, CA); Guangyi Wang (Carlsbad, CA); David Bernard Smith (San Mateo, CA)
Assignee: Janssen Pharmaceutica NV
C07H19/10A61K31/7076A61P31/14C07H19/06C07H19/16C07H19/173C07H19/20C07H19/207C07H19/213
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Quick Facts
Patent No.
US 11,485,753
App. No.
17/063,545
Granted
Nov 1, 2022
Kind
B2
Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Claims (39)

1. A pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, having the structure:

wherein:

B 1 is selected from the group consisting of

R 1 is selected from the group consisting of an unsubstituted C 1-6 alkyl and an unsubstituted C 2-6 alkynyl;

each is absent;

R 2 is fluoro;

R P is absent;

R 3 is OH;

R 4 is hydrogen or

R 5A is selected from the group consisting of OH,

R 5B is selected from the group consisting of an OH, —O-unsubstituted phenyl, —O-unsubstituted naphthyl,

R 6B and R 6C are each independently selected from the group consisting of hydrogen and an unsubstituted C 1-6 alkyl;

R 11A , R 12A , R 11B and R 12B are each hydrogen;

R 13 is selected from the group consisting of an unsubstituted C 1-6 alkyl and an unsubstituted C 3-6 cycloalkyl;

R 14 and R 15 are each independently selected from the group consisting of hydrogen and an unsubstituted C 1-6 alkyl;

R 13A and R 13B are each an unsubstituted —O—C 1-4 alkyl;

n is 0 or 1;

R 9 , R 10 and R 11 are each hydrogen; and

Z 1 , Z 1A and Z 1B are each O,

and a pharmaceutically acceptable carrier, diluent, excipient or combination thereof.

2. The pharmaceutical composition of claim 1 , wherein R 1 is an unsubstituted C 1-6 alkyl.

3. The pharmaceutical composition of claim 1 , wherein R 1 is methyl.

4. The pharmaceutical composition of claim 1 , wherein R 1 is ethynyl.

5. The pharmaceutical composition of claim 1 , wherein R 4 is hydrogen.

6. The pharmaceutical composition of claim 1 , wherein R 4 is

7. The pharmaceutical composition of claim 6 , wherein R 5B is an —O-unsubstituted phenyl; and R 5A is

8. The pharmaceutical composition of claim 6 , wherein R 5A is

9. The pharmaceutical composition of claim 6 , wherein R 5A is

10. The pharmaceutical composition of claim 6 , wherein R 5A is

11. The pharmaceutical composition of claim 10 , wherein R 13A and R 13B are each —O-isopropyl.

12. The pharmaceutical composition of claim 1 , wherein B 1 is

13. The pharmaceutical composition of claim 1 , wherein R 6C is ethyl.

14. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has a structure selected from the group consisting of:

15. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has the structure

16. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has the structure

17. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has a structure selected from the group consisting of:

18. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has a structure selected from the group consisting of:

19. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has a structure selected from the group consisting of:

20. The pharmaceutical composition of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, has the structure

Assignments (2)
CHANGE OF NAME Recorded Jun 7, 2022
From: JANSSEN BIOPHARMA, INC
To: JANSSEN BIOPHARMA, LLC
Reel/Frame 060300/0694 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 7, 2022
From: JANSSEN BIOPHARMA, LLC
To: JANSSEN PHARMACEUTICA NV
Reel/Frame 060300/0750 →
Continuity (8)
Continuation 16692858 · Nov 22, 2019
Continuation 16161705 · Oct 16, 2018
Continuation 15256337 · Sep 2, 2016
Continuation 14836896 · Aug 26, 2015
Continuation 14135484 · Dec 19, 2013
Provisional Application 61890125 · Oct 11, 2013
Provisional Application 61745466 · Dec 21, 2012
Related Publication 20210139523A1 · May 13, 2021